Fluorine Luo The Fungus Nitrile Synthesis And Its Analogues

As microbicides with high efficiency, low toxicity and high selectivity, Fludioxonil and its analogues are widely used abroad, however, it is a new product in our country. Development of fludioxonil synthesis technology is expected to bring huge commercial value.In this paper, the synthesis of fludioxonil and its analogues were investigated. A optimum synthetic route was determined based on the comparison of different synthetic methods in literatures.2,2-Difluoro-1,3-benzodioxole-4-carboxaldehyde and cyanoacetamide were adopted as the starting materials. A Knoevenagel reaction occured under alkaline condition to give cinnamon amide compounds as the intermediates which then reacted with tosmic in alkaline solution through Michael addition reaction to get target product. And the effects of reaction conditions had also been studied such as materials rate, solvent, reacting temperature, reacting time, etc. to get optimum technological parameters. The chemical structures and purity of these products and their intermediates were confirmed by HNMR, IR and HPLC. Single crystals of fludioxonil and some analogues were obtained for the first time, which further characterized their structures by X-Ray diffraction analysis.